Thanks to the ability to suppress the proliferation and to kill tumour cells, several studies have shown the anti-cancer effects of curcumin (CUR) and its derivatives, i.e. diacetylcurcumin (DAC) and bis-dehydroxycurcumin (bDHC). This study is focused onto the development of curcuminoid complexes with gallium-68 employed as potential new radio-labelled probes to detect neoplastic tissues through imaging techniques such as positron emission tomography. To this purpose, the uptake of three Ga-curcuminoid complexes, namely Ga(CUR)2+, Ga(DAC)2+, Ga(bDHC)2+, by various tumour cell lines was compared with the uptake of the same compounds by normal human lymphocytes by flow cytometry using the intrinsic fluorescence of the curcuminoids. Ga(CUR)2+, and particularly Ga(DAC)2+, showed a higher uptake by colorectal carcinoma (HT29) and lymphoma (K562) cell lines than lymphocytes, while the uptake of Ga(bDHC)2+ was higher in lymphocytes than in all the other cell lines. Based on the fluorescence data, Gallium-68 labelled complexes were then tested in HT29 cell line. 68Ga(DAC)2+ showed the highest uptake by HT29 cells (higher internalization with a lower externalization) and the highest affinity. The obtained results are promising and the findings foster further investigation on the development of curcumin-metal-based radiopharmaceuticals.

Uptake of Ga-curcumin derivatives in different cancer cell lines: toward the development of new potential 68Ga-labelled curcuminoids-based radiotracers for tumour imaging / Rubagotti, Sara; Croci, Stefania; Ferrari, Erika; Orteca, Giulia; Iori, Michele; Capponi, Pier C.; Versari, Annibale; Asti, Mattia. - In: JOURNAL OF INORGANIC BIOCHEMISTRY. - ISSN 0162-0134. - 173:(2017), pp. 113-119. [10.1016/j.jinorgbio.2017.05.002]

Uptake of Ga-curcumin derivatives in different cancer cell lines: toward the development of new potential 68Ga-labelled curcuminoids-based radiotracers for tumour imaging.

FERRARI, Erika;ORTECA, GIULIA;
2017

Abstract

Thanks to the ability to suppress the proliferation and to kill tumour cells, several studies have shown the anti-cancer effects of curcumin (CUR) and its derivatives, i.e. diacetylcurcumin (DAC) and bis-dehydroxycurcumin (bDHC). This study is focused onto the development of curcuminoid complexes with gallium-68 employed as potential new radio-labelled probes to detect neoplastic tissues through imaging techniques such as positron emission tomography. To this purpose, the uptake of three Ga-curcuminoid complexes, namely Ga(CUR)2+, Ga(DAC)2+, Ga(bDHC)2+, by various tumour cell lines was compared with the uptake of the same compounds by normal human lymphocytes by flow cytometry using the intrinsic fluorescence of the curcuminoids. Ga(CUR)2+, and particularly Ga(DAC)2+, showed a higher uptake by colorectal carcinoma (HT29) and lymphoma (K562) cell lines than lymphocytes, while the uptake of Ga(bDHC)2+ was higher in lymphocytes than in all the other cell lines. Based on the fluorescence data, Gallium-68 labelled complexes were then tested in HT29 cell line. 68Ga(DAC)2+ showed the highest uptake by HT29 cells (higher internalization with a lower externalization) and the highest affinity. The obtained results are promising and the findings foster further investigation on the development of curcumin-metal-based radiopharmaceuticals.
2017
10-mag-2017
173
113
119
Uptake of Ga-curcumin derivatives in different cancer cell lines: toward the development of new potential 68Ga-labelled curcuminoids-based radiotracers for tumour imaging / Rubagotti, Sara; Croci, Stefania; Ferrari, Erika; Orteca, Giulia; Iori, Michele; Capponi, Pier C.; Versari, Annibale; Asti, Mattia. - In: JOURNAL OF INORGANIC BIOCHEMISTRY. - ISSN 0162-0134. - 173:(2017), pp. 113-119. [10.1016/j.jinorgbio.2017.05.002]
Rubagotti, Sara; Croci, Stefania; Ferrari, Erika; Orteca, Giulia; Iori, Michele; Capponi, Pier C.; Versari, Annibale; Asti, Mattia
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11380/1139161
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